Synthesis and characterization of a novel polydepsipeptide contained tri-block copolymer (mPEG–PLLA–PMMD) as self-assembly micelle delivery system for paclitaxel
2012
Zhao, Yanlei | Li, Juan | Yu, Hua | Wang, Guangji | Liu, Wen
A series of biodegradable polydepsipeptides based new triblock copolymers, poly (ethylene glycol)-poly(l-lactide)–poly(3(S)-methyl-morpholine-2,5-dione) (mPEG–PLLA–PMMD) have been synthesized and characterized as self-assembly micelle delivery system for paclitaxel (PTX). Compared to the mPEG₂₀₀₀–PLLA₂₀₀₀ diblock copolymers, the triblock copolymers present more benefits such as lower CMC value, positive-shifted zeta potential, better drug loading efficiency and stability. Among the triblock polymers, mPEG₂₀₀₀–PLLA₂₀₀₀–PMMD₁₄₀₀ micelles present low cytotoxicity and promote the anti-cancer activity of PTX on A-549 and HCT-116cells. In addition, mPEG₂₀₀₀–PLLA₂₀₀₀–PMMD₁₄₀₀ micelles prolongs the circulation time of PTX in rat after i.v. injection (5mg/kg) than that of mPEG₂₀₀₀–PLLA₂₀₀₀ micelles and Taxol®. The half life (t₁/₂ᵦ), mean residence time (MRT), AUC₀–∞ and clearance (CL) for PTX-loaded mPEG₂₀₀₀–PLLA₂₀₀₀–PMMD₁₄₀₀ micelles are determined to be 1.941h, 2.683h, 5.220μg/mLh (1.8-fold to mPEG₂₀₀₀–PLLA₂₀₀₀ group), 0.967L/hkg⁻¹, respectively. In conclusion, mPEG₂₀₀₀–PLLA₂₀₀₀–PMMD₁₄₀₀ copolymer could be developed as one of the promising vectors to anti-cancer agents for chemotherapeutics.
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